Chemistry Reference
In-Depth Information
[6] Way, J. (2000). Covalent modification as a strategy to block protein-protein interactions with
small-molecule drugs. Curr. Opin. Chem. Biol . 4 , 40-46.
[7] Rademann, J. (2004). Organic protein chemistry: drug discovery through the chemical
modification of proteins. Angew. Chem. Int. Ed . 43 , 4554-4556.
[8] Rishton, G.M. (2003). Nonleadlikeness and leadlikeness in biochemical screening. DrugDiscov.
Today 8 , 86-96.
[9] McGovern, S. L., Helfand, B. T., Feng, B. and Shoichet, B. K. (2003). A specific mechanism of
nonspecific inhibition. J. Med. Chem . 46 , 4265-4272.
[10] Tethering is a registered service mark of Sunesis Pharmaceuticals, Inc., for its fragment-based
drug discovery.
[11] Erlanson, D. A., Braisted, A. C., Raphael, D. R., Randal, M., Stroud, R. M., Gordon, E. M. and
Wells, J. A. (2000). Site-directed ligand discovery. Proc. Natl. Acad. Sci. USA 97 , 9367-9372.
[12] Erlanson, D. A., Wells, J. A. and Braisted, A. C. (2004). Tethering: fragment-based drug
discovery. Annu. Rev. Biophys. Biomol. Struct . 33 , 199-223.
[13] Nelson, B. H. and Willerford, D. M. (1998). Biology of the interleukin-2 receptor. Adv.
Immunol . 70 , 1-81.
[14] Tilley, J. W., Chen, L., Fry, D. C., Emerson, S. D., Powers, G. D., Biondi, D., Varnell, T., Trilles,
R., Guthrie, R., Mennona, F., Kaplan, G., LeMahieu, R. A., Carson, M., Han, R.-J., Liu, C.-M.,
Palermo, R. and Ju, G. (1997). Identification of a small molecule inhibitor of the IL-2/IL-2Ra
receptor interaction which binds to IL-2. J. Am. Chem. Soc . 119 , 7589-7590.
[15] Arkin, M. R., Randal, M., DeLano, W. L., Hyde, J., Luong, T. N., Oslob, J. D., Raphael, D. R.,
Taylor, L., Wang, J., McDowell, R. S., Wells, J. A. and Braisted, A. C. (2003). Binding of small
molecules to an adaptive protein-protein interface. Proc. Natl. Acad. Sci. USA 100 , 1603-1608.
[16] Braisted, A. C., Oslob, J. D., Delano, W. L., Hyde, J., McDowell, R. S., Waal, N., Yu, C.,
Arkin, M. R. and Raimundo, B. C. (2003). Discovery of a potent small molecule IL-2 inhibitor
through fragment assembly. J. Am. Chem. Soc . 125 , 3714-3715.
[17] Raimundo, B. C., Oslob, J. D., Braisted, A. C., Hyde, J., McDowell, R. S., Randal, M.,
Waal, N. D., Wilkinson, J., Yu, C. H. and Arkin, M. R. (2004). Integrating fragment assembly
and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2:
an approach for inhibiting protein-protein interactions. J. Med. Chem . 47 , 3111-3130.
[18] Thanos, C. D., Randal, M. and Wells, J. A. (2003). Potent small-molecule binding to a dynamic
hot spot on IL-2. J. Am. Chem. Soc . 125 , 15280-15281.
[19] Buck, E., Bourne, H. andWells, J. (2005). Site-specific disulfide capture of agonist and antgonist
peptides on the C5a receptor. J. Biol. Chem . 280 , 4009-4012.
[20] Buck, E. and Wells, J. A. (2005). Disulfide trapping to localize small-molecule agonists and
antagonists for a G protein-coupled receptor. Proc. Natl. Acad. Sci. USA 102 , 2719-2724.
[21] Erlanson, D. A., Lam, J. W., Wiesmann, C., Luong, T. N., Simmons, R. L., DeLano, W. L.,
Choong, I. C., Burdett, M. T., Flanagan, W. M., Lee, D., Gordon, E. M. and O'Brien, T. (2003).
In situ assembly of enzyme inhibitors using extended tethering. Nat. Biotechnol . 21 , 308-314.
[22] Allen, D. A., Pham, P., Choong, I. C., Fahr, B., Burdett, M. T., Lew, W., DeLano, W. L.,
Gordon, E. M., Lam, J. W., O'Brien, T. and Lee, D. (2003). Identification of potent and novel
small-molecule inhibitors of caspase-3. Bioorg. Med. Chem. Lett . 13 , 3651-3655.
[23] Choong, I. C., Lew, W., Lee, D., Pham, P., Burdett, M. T., Lam, J. W., Wiesmann, C., Luong, T.
N., Fahr, B., DeLano, W. L., McDowell, R. S., Allen, D. A., Erlanson, D. A., Gordon, E. M. and
O'Brien, T. (2002). Identification of potent and selective small-molecule inhibitors of caspase-
3 through the use of extended tethering and structure-based drug design. J. Med. Chem . 45 ,
5005-5022.
[24] Fahr, B. T., O'Brien, T., Pham, P., Waal, N. D., Baskaran, S., Raimundo, B. C., Lam, J. W.,
Sopko, M. M., Purkey, H. E. and Romanowski, M. J. (2006). Tethering identifies fragment that
yields potent inhibitors of human caspase-1. Bioorg. Med. Chem. Lett . 16 , 559-62.
Search WWH ::




Custom Search